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L-778,123
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
L-778,123图片
CAS NO:183499-57-2
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
A dual inhibitor of FTase and GGTase I
Cas No.183499-57-2
Canonical SMILESClC1=CC(N2C(CN(CC3=CN=CN3CC4=CC=C(C#N)C=C4)CC2)=O)=CC=C1
分子式C22H20ClN5O
分子量405.9
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:9): 0.1 mg/ml,Ethanol: 10 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

L-778,123 is a dual inhibitor of farnesyl transferase (FTase; IC50= 2 nM) and geranylgeranyl transferase type I (GGTase I; IC50= 98 nM).1It inhibits prenylation of the FTase and GGTase I substrates HDJ2 and Rap1a in PSN-1 pancreatic tumor cells (EC50s = 92 and 6,760 nM, respectively). L-778,123 (1-300 μM) also inhibits prenylation of the oncogenic protein Ki-Ras in PSN-1 cells in a concentration-dependent manner.Ex vivo, L-778,123 (35-50 mg/kg per day) reduces HDJ2 and Rap1a prenylation in dog peripheral blood mononuclear cells (PBMCs) but has no effect on Ki-Ras prenylation in patient-derived PBMCs. L-778,123 inhibits lectin-induced expression of the T cell activation markers CD71 and CD25 on human PMBCs (IC50s = 6.48 and 84.1 μM, respectively) and inhibits IL-2-induced proliferation of CTLL2 cells (IC50= 0.81 μM).2

1.Lobell, R.B., Liu, D., Buser, C.A., et al.Preclinical and clinical pharmacodynamic assessment of L-778,123, a dual inhibitor of farnesyl:protein transferase and geranylgeranyl:protein transferase type-IMol. Cancer Ther.1(9)747-758(2002) 2.Si, M.-S., Reitz, B.A., and Borie, D.C.Inhibition of lymphocyte activation and function by the prenylation inhibitor L-778,123Invest New Drugs23(1)21-29(2005)